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FA Bucci; An In Vivo Comparison of the Ocular Absorption of Levofloxacin versus Ciprofloxacin Prior to Phacoemulsification . Invest. Ophthalmol. Vis. Sci. 2002;43(13):1579.
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Purpose: To compare aqueous humor concentrations of levefloxacin (levo) versus ciprofloxacin (cipro) when used as prophylactic medications prior to phacoemulsification. Methods: 93 patients were randomized to receive either QuixinTM (0.5% levofloxacin, Santen Inc.) or Ciloxan® (0.3% ciprofloxacin, Alcon Laboratories, Inc.) prior to phacoemulsification. Patients were further randomized to one of three dosing regimens: (A) QID x 2d preop; (B) Q10 min x 5 during the hour immediately preceding surgery; or (C) a combination of A and B. Aqueous samples (0.1mL) were obtained immediately prior to surgery and the concentrations of levo and cipro were measured using an HPLC/MS procedure. Results: Although the concentration of active drug in Quixin is approximately 1.7-fold higher than that of Ciloxan, the concentrations of levo in the aqueous humor were 4 to 7 times higher than those of cipro; these differences were statistically significant (p<0.001). Dosing regimen B delivered significantly more drug to the aqueous humor than dosing regimen A for both levo (p<0.001) and cipro (p=0.004). Dosing regimen C delivered significantly more drug to the aqueous humor than dosing regimen B for levo (p=0.05), but not for cipro (p=0.384). With dosing regimen C, the concentration of levo in the aqueous humor was above the MIC90 for most common ocular bacterial pathogens, including staphylococcus and streptococcus species. Cipro did not achieve such concentrations in any treatment group. Conclusions: In this study, the ocular absorption of levo was between 4 to 7 times greater than cipro; these differences were statistically and clinically significant. The pulsed delivery regimen of Q10 min x 5 yielded almost 4 times as much penetration of levo compared to QID x 2d preop. Combination dosing (QID x 2d/Q10 min x 5) yielded an additional 50% penetration of levo compared to the Q10 min x 5 group. The difference in penetration of levo versus cipro increased with increasing amounts of medication used. Therapeutic (above the MIC90) concentrations of drug in the aqueous humor for both staphylococcus and streptococcus were demonstrated after dosing with Quixin but not Ciloxan. Treatment Regimen View OriginalDownload SlideView OriginalDownload Slide
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